Thiopurine methyltransferase: structure-activity relationships for benzoic acid inhibitors and thiophenol substrates

Twenty-seven substituted benzoic acids have been studied as inhibitors of partially purified human renal thiopurine methyltransferase (TPMT). Quantitative structure-activity relationship (QSAR) analysis resulted in the following equation: pI50 = 1.25( +/- 0.53)pi'3 + 0.73( +/- 0.38)MR3,4 + 2.92...

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Veröffentlicht in:	Journal of medicinal chemistry 1986-03, Vol.29 (3), p.354-358
Hauptverfasser:	Ames, Matthew M, Selassie, Cynthia Dias, Woodson, Lee C, Van Loon, Jon A, Hansch, Corwin, Weinshilboum, Richard M
Format:	Artikel
Sprache:	eng
Schlagworte:	Benzoates - pharmacology Biological and medical sciences General pharmacology Humans Kidney - enzymology Kinetics Medical sciences Methyltransferases - antagonists & inhibitors Methyltransferases - metabolism Models, Chemical Pharmacology. Drug treatments Phenols - metabolism Physicochemical properties. Structure-activity relationships Structure-Activity Relationship Sulfhydryl Compounds
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